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1. 发明申请

US20110160208A1 DIARYL-SUBSTITUTED FIVE-MEMBERED HETEROCYCLE DERIVATIVE 审中-公开
标题翻译： DIARYL取代的五分子杂交衍生物
公开(公告)号：US20110160208A1
公开(公告)日：2011-06-30
申请号：US13041848
申请日：2011-03-07
申请人： Yukari Hirata , Satoru Ito , Hiroshi Kawamoto , Toshifumi Kimura , Yasushi Nagatomi , Hisashi Ohta , Akio Sato , Atsushi Satoh , Gentaroh Suzuki
发明人： Yukari Hirata , Satoru Ito , Hiroshi Kawamoto , Toshifumi Kimura , Yasushi Nagatomi , Hisashi Ohta , Akio Sato , Atsushi Satoh , Gentaroh Suzuki
IPC分类号： A61K31/4709 , C07D401/10 , C07D249/06 , A61K31/4192 , C07D417/10 , A61K31/428 , C07D403/10 , C07D405/10 , A61K31/497 , C07D471/04 , A61K31/444 , C07D491/052 , A61K31/4725 , C07D401/04 , A61K31/4439 , C07D413/14 , A61K31/5377 , C07D401/14 , A61K31/517 , C07D487/04 , A61P25/08 , A61P25/04 , A61P29/00 , A61P25/00 , A61P9/10 , A61P25/18 , A61P25/22 , A61P25/30 , A61P25/16 , A61P1/00
CPC分类号： C07D471/04 , C07D249/06 , C07D401/04 , C07D401/14 , C07D403/04 , C07D405/14 , C07D409/14 , C07D417/14 , C07D491/04 , C07D513/04
摘要： The present invention provides the compounds represented by formula (I): or pharmaceutical salts thereof, wherein: X1 represents oxygen atoms and the like, X2 represents nitrogen atoms and the like, X3 represents nitrogen atoms and the like, X4 represents nitrogen atoms and the like, R1 represents formula (II-1): wherein X5 represents sulfur atoms and the like, A1 represents carbon atoms and the like, A2 represents nitrogen atoms and the like and A ring represents phenyl group and the like, having mGluR1 inhibiting effect, and being useful for preventing or treating convulsion, acute pain, inflammatory pain, chronic pain, brain disorder such as cerebral infarction or transient ischemick attack, psychotic disorder such as schizophrenia, anxiety, drug dependence, Parkinson's disease, or gastrointestinal disorder.
摘要翻译：本发明提供由式（I）表示的化合物或其药用盐，其中：X1表示氧原子等，X2表示氮原子等，X3表示氮原子等，X4表示氮原子， R 1表示式（II-1）：其中X 5表示硫原子等，A 1表示碳原子等，A 2表示氮原子等，A表示具有mGluR1抑制作用的苯基等，并且可用于预防或治疗惊厥，急性疼痛，炎性疼痛，慢性疼痛，脑梗塞如脑梗塞或短暂性脑缺血发作，精神病如精神分裂症，焦虑症，药物依赖性，帕金森病或胃肠道疾病。

2. 发明申请

US20100261699A1 N-PYRAZOLE-2-PYRIDINE CARBOXAMIDE DERIVATIVE 审中-公开
标题翻译： N-吡咯-2-吡啶酰胺衍生物
公开(公告)号：US20100261699A1
公开(公告)日：2010-10-14
申请号：US12746567
申请日：2008-12-15
申请人： Noriaki Hashimoto , Teruyuki Nishimura , Yufu Sagara
发明人： Noriaki Hashimoto , Teruyuki Nishimura , Yufu Sagara
IPC分类号： A61K31/4439 , C07D401/14 , A61P3/10
CPC分类号： A61K31/155 , A61K31/427 , A61K31/44 , A61K31/4439 , A61K31/444 , A61K38/28 , A61K38/31 , C07D401/14 , A61K2300/00
摘要： The present invention relates to a compound represented by the formula: or a pharmaceutically acceptable salt thereof, wherein R1 and R2 are each independently a lower alkyl group, X is CH or the like, and X1 is an aminoalkoxy group or the like, which has a glucokinase-activating effect and thus is useful in the treatment of diabetes, obesity, and the like.
摘要翻译：本发明涉及由下式表示的化合物或其药学上可接受的盐，其中R1和R2各自独立地为低级烷基，X为CH等，X1为氨基烷氧基等，其具有葡糖激酶活化作用，因此可用于治疗糖尿病，肥胖症等。

3. 发明申请

US20100130559A1 NOVEL PHENYL-ISOXAZOL-3-OL DERIVATIVE 有权
标题翻译：新型PHENYL-ISOXAZOL-3-OL DERIVATIVE
公开(公告)号：US20100130559A1
公开(公告)日：2010-05-27
申请号：US12516025
申请日：2007-11-29
申请人： Noriaki Hashimoto , Yasuhiro Sasaki , Chisato Nakama , Makoto Ishikawa
发明人： Noriaki Hashimoto , Yasuhiro Sasaki , Chisato Nakama , Makoto Ishikawa
IPC分类号： A61K31/4439 , C07D413/12 , C07D417/12 , A61K31/422 , A61K31/427 , C07D261/02 , A61K31/421 , A61P3/04 , A61P3/06 , A61P3/10
CPC分类号： C07D261/12 , C07D413/04 , C07D413/12 , C07D417/12
摘要： The present invention relates to a compound represented by formula (I), which has a GPR120 agonist action and thus is useful for treatment of diabetes mellitus or hyperlipidemia, or a pharmaceutically acceptable salt thereof. In the formula, (AA) represents a phenyl or the like, which may be substituted with a lower alkoxy group or the like; (BB) represents a divalent group or the like, derived by removal of two hydrogen atoms from a benzene which may be substituted with a halogen atom or the like; X represents a spacer having a main chain composed of 1-8 carbon atoms wherein 1-3 carbon atoms in the main chain may be substituted with an oxygen atom or the like; and Y represents a hydrogen atom or the like.
摘要翻译：本发明涉及由式（I）表示的化合物，其具有GPR120激动剂作用，因此可用于治疗糖尿病或高脂血症或其药学上可接受的盐。式中，（AA）表示可以被低级烷氧基等取代的苯基等，（BB）表示通过从可以被卤素原子等取代的苯中除去两个氢原子得到的二价基团等; X表示具有由1-8个碳原子构成的主链的间隔基，其中主链中的1-3个碳原子可以被氧原子等取代; Y表示氢原子等。

4. 发明申请

US20090258871A1 Aza-Substituted Spiro Derivatives 有权
标题翻译：氮杂取代的螺衍生物
公开(公告)号：US20090258871A1
公开(公告)日：2009-10-15
申请号：US12084817
申请日：2006-11-10
申请人： Makoto Jitsuoka , Nagaaki Sato , Daisuke Tsukahara
发明人： Makoto Jitsuoka , Nagaaki Sato , Daisuke Tsukahara
IPC分类号： A61K31/5377 , C07D221/20 , A61K31/438 , C07D295/00 , C07D239/24 , A61K31/506 , A61P3/00 , A61P25/00
CPC分类号： C07D491/10
摘要： A compound of the following formula (I) or its pharmaceutically-acceptable salt is provided: [wherein X, Y, Z and W each independently represent a methine group or a nitrogen atom, provided that a case where all of X, Y, Z and W are methine group; A represents —O— or the like, B represents —C(O)— or the like, D represent —(CH2)m2-, —O— or the like, and m2 represents 0 or 1; Q represents a methine group or a nitrogen atom; and R represents a group represented by the following formula (II-1) (wherein R6, R7 and R8 independently represent a lower alkyl group or the like].
摘要翻译：提供下式（I）的化合物或其药学上可接受的盐：[其中X，Y，Z和W各自独立地表示次甲基或氮原子，条件是X，Y，Z全部为 W是次甲基; A表示-O-等，B表示-C（O） - 等，D表示 - （CH2）m2-，-O-等，m2表示0或1; Q表示次甲基或氮原子; 并且R表示由下式（II-1）表示的基团（其中R 6，R 7和R 8独立地表示低级烷基等）。

5. 发明申请

US20090209562A1 Fused ring 4-oxopyrimidine derivative 有权
公开(公告)号：US20090209562A1
公开(公告)日：2009-08-20
申请号：US12378163
申请日：2009-02-11
申请人： Tsuyoshi Nagase , Nagaaki Sato , Akio Kanatani , Shigeru Tokita
发明人： Tsuyoshi Nagase , Nagaaki Sato , Akio Kanatani , Shigeru Tokita
IPC分类号： A61K31/517 , C07D239/88 , A61P25/00
CPC分类号： C07D239/91 , A61K31/517 , A61K31/55 , A61K45/06 , C07D401/12 , C07D403/12 , C07D471/04 , C07D487/08 , A61K2300/00
摘要： The present invention provides a compound represented by formula (I) below, or a pharmaceutically acceptable salt thereof, which, having histamine H3 receptor antagonist or inverse agonist activity, is useful in the prophylaxis or therapy of metabolic diseases, circulatory diseases, or nervous system diseases. [where, for example, Ar is a divalent group formed by eliminating two hydrogen atoms from benzene, X1 is a nitrogen atom, sulfur atom or oxygen atom, R1 is a 5- to 6-membered heteroaryl group, Ring A is a 5- to 6-membered heteroaryl ring, R2 and R3 are amino groups or alkylamino groups, and X2 is represented by formula (II): (where R4 and R5 are lower alkyl groups, and n is an integer from 2 to 4).]

6. 发明授权

US07531668B2 2-arylcarboxamide-nitrogenous heterocycle compound 失效
标题翻译： 2-芳基羧酰胺 - 含氮杂环化合物
公开(公告)号：US07531668B2
公开(公告)日：2009-05-12
申请号：US11663038
申请日：2005-09-30
申请人： Takao Suzuki , Minoru Moriya , Shunji Sakuraba , Sayaka Mizutani , Hisashi Iwaasa , Akio Kanatani
发明人： Takao Suzuki , Minoru Moriya , Shunji Sakuraba , Sayaka Mizutani , Hisashi Iwaasa , Akio Kanatani
IPC分类号： C07D235/12 , C07D209/12 , C07D211/06 , C07D401/12 , C07D291/04 , C07D291/06 , C07D279/02 , C07D279/06 , C07D279/12 , C07D265/02 , C07D265/06 , C07D265/30 , C07D257/04 , C07D257/08 , C07D251/04 , C07D237/04
CPC分类号： C07D209/42 , C07D235/24 , C07D401/12
摘要： A compound represented by the formula [I]: [wherein R1 and R2 are the same or different and each represents C1-6 alkyl, C3-8 cycloalkyl, et al; R3a, R3b, and R4 are the same or different and each represents hydrogen, C1-6 alkyl, et al; X represents —N—, —CH—, et al; Y1 represents a single bond, C1-3 alkylene, et al; Y2 represents C1-4 alkylene, oxy(C1-4 alkylene), et al; Ar1 represents a monocyclic aromatic carbocyclic group, monocyclic aromatic heterocyclic group, et al; and Ar2 represents a 5- or 6-membered aromatic carbocyclic group, aromatic heterocyclic group, et al]. This compound functions as a melanin-concentrating hormone receptor antagonist and is useful as, e.g., a therapeutic agent for obesity, et al.
摘要翻译：由式[I]表示的化合物：其中R 1和R 2相同或不同，各自表示C 1-6烷基，C 3-8环烷基等; R3a，R3b和R4相同或不同，各自表示氢，C1-6烷基等; X表示-N-，-CH-等; Y1表示单键，C1-3亚烷基等; Y2代表C1-4亚烷基，氧基（C1-4亚烷基）等; Ar 1表示单环芳族碳环基团，单环芳族杂环基团等; 和Ar 2表示5或6元芳族碳环基团，芳族杂环基团等。该化合物起着黑色素浓缩激素受体拮抗剂的作用，可用作例如肥胖症的治疗剂等。

7. 发明授权

US07510833B2 Method for examining obesity or leanness 失效
标题翻译：检查肥胖或瘦身的方法
公开(公告)号：US07510833B2
公开(公告)日：2009-03-31
申请号：US10548772
申请日：2004-03-12
申请人： Hidehito Kotani , Hiraku Itadani , Hiromitsu Araki , Kazuhiko Takahashi , Satoshi Mashiko , Akane Ishihara , Akio Kanatani
发明人： Hidehito Kotani , Hiraku Itadani , Hiromitsu Araki , Kazuhiko Takahashi , Satoshi Mashiko , Akane Ishihara , Akio Kanatani
IPC分类号： C12Q1/68 , C07H21/04 , C12P19/34
CPC分类号： C12Q1/6883 , C12Q2600/136 , C12Q2600/156 , C12Q2600/158 , G01N33/5088 , G01N33/6893 , G01N2800/044 , G01N2800/52
摘要： In the examination of obesity or leanness, the examination is based on the expression level of the MCP-1 gene or the MCP-1 protein in a tissue or cell analyte, or on the polymorphism in the gene. In the evaluation of compounds, including screening for therapeutic agents for obesity or leanness, the properties of the MCP-1 gene or the MCP-1 protein are utilized to carry out the evaluation.
摘要翻译：在检查肥胖或瘦身时，检查是基于组织或细胞分析物中MCP-1基因或MCP-1蛋白的表达水平，或基于该基因的多态性。在化合物的评价中，包括筛选肥胖或瘦身的治疗剂，使用MCP-1基因或MCP-1蛋白的性质进行评价。

8. 发明授权

US07439535B2 Process for exchanging functional groups by halogen-metal exchange reaction 失效
标题翻译：通过卤素 - 金属交换反应交换官能团的方法
公开(公告)号：US07439535B2
公开(公告)日：2008-10-21
申请号：US11077292
申请日：2005-03-11
申请人： Takehiko Iida , Toshihiro Wada , Toshiaki Mase
发明人： Takehiko Iida , Toshihiro Wada , Toshiaki Mase
IPC分类号： C07F3/02
CPC分类号： C07D213/84 , C07C45/004 , C07C45/45 , C07D213/61 , C07D333/28 , C07F3/02 , C07F7/0827 , C07C47/55
摘要： A method by which a halogen atom of a halogen compound can be efficiently replaced with an electrophilic group.Also provided are: a reagent for converting a functional group through a halogen-metal exchange reaction, characterized by comprising either a mixture of a magnesium compound represented by the formula R1—Mg—X (I) (wherein R1 represents a halogen atom or an optionally substituted hydrocarbon residue; and X1 represents a halogen atom) and an organolithium compound represented by the formula R2—Li (II)(wherein R2 represents an optionally substituted hydrocarbon residue) or a product of the reaction of the magnesium compound with the organolithium compound; and a process for producing with the reagent a compound in which a halogen atom of a halogen compound has been replaced with an electrophilic group.
摘要翻译：可以用亲电子基团有效地代替卤素化合物的卤素原子的方法。还提供：用于通过卤素 - 金属交换反应转化官能团的试剂，其特征在于包含由式R 1 -Mg-X（I）表示的镁化合物的混合物（其中R 1表示卤素原子或任选取代的烃残基; X 1表示卤素原子）和由式R 2表示的有机锂化合物，（II）（其中R 2表示任选取代的烃残基）或镁化合物与有机锂化合物的反应的产物; 以及用该试剂制备其中卤素化合物的卤素原子已被亲电子基团取代的化合物的方法。

9. 发明授权

US07388010B2 Quinoxalinone derivatives 失效
标题翻译：喹喔啉酮衍生物
公开(公告)号：US07388010B2
公开(公告)日：2008-06-17
申请号：US10532677
申请日：2003-10-27
申请人： Hiroshi Hirai , Nobuhiko Kawanishi , Masaaki Hirose , Tetsuya Sugimoto , Kaori Kamijyo , Jun Shibata , Kouta Masutani
发明人： Hiroshi Hirai , Nobuhiko Kawanishi , Masaaki Hirose , Tetsuya Sugimoto , Kaori Kamijyo , Jun Shibata , Kouta Masutani
IPC分类号： A61K31/498 , A61P35/00 , C07D487/00
CPC分类号： C07D487/18 , A61K31/4995 , A61K31/506 , A61K31/517 , A61K31/5377 , A61K31/55 , C07D498/18 , C07D498/22 , C07D515/18 , C07D515/22
摘要： A quinoxalinone derivative of the formula (I): or a pharmaceutically acceptable salt or ester thereof, wherein; X is NH, S or the like; Y is O or the like; the partial structure is, for example, the formula: B1, B2, . . . , Bn−1 and Bn, (in which n is 4, 5 or 6) are each independently CH, N or the like; B′1, B′2, . . . , B′n−1 and B′n (in which n is 4, 5 or 6) are each independently hydrogen or the like; and R is hydrogen, lower alkyl or the like.
摘要翻译：式（I）的喹喔啉酮衍生物或其药学上可接受的盐或酯，其中： X是NH，S等; Y为O等; 该部分结构例如是以下公式：B 1，B 2，...。。。（其中n为4,5或6）各自独立地为CH，N等;其中n为4或5或6。 B'1，B'2，...，。。，其中n为4,5或6个，各自独立地为氢等;其中n为4或5或6。和R是氢，低级烷基等。

10. 发明申请

US20080125429A1 Aryloxy-Substituted Benzimidazole Derivatives 有权
标题翻译：芳氧基取代的苯并咪唑衍生物
公开(公告)号：US20080125429A1
公开(公告)日：2008-05-29
申请号：US11666555
申请日：2005-11-01
申请人： Noriaki Hashimoto , Keiji Takahashi , Chisato Nakama , Yoshio Ogino , Fumiko Sakai , Teruyuki Nishimura , Jun-ichi Eiki
发明人： Noriaki Hashimoto , Keiji Takahashi , Chisato Nakama , Yoshio Ogino , Fumiko Sakai , Teruyuki Nishimura , Jun-ichi Eiki
IPC分类号： A61K31/5377 , C07D213/02 , C07D221/00 , C07D239/06 , C07D241/10 , C07D295/00 , A61P3/10 , A61K31/4439 , A61K31/4545 , A61K31/444 , A61K31/506 , A61K31/497
CPC分类号： A61K38/31 , A61K31/155 , A61K31/4439 , A61K31/444 , A61K31/4545 , A61K31/497 , A61K31/506 , A61K38/28 , A61K45/06 , C07D401/04 , C07D401/14 , C07D413/06 , C07D413/14 , A61K2300/00
摘要： A glucokinase activator is provided; and a treatment and/or a preventive for diabetes, or a treatment and/or a preventive for diabetes such as retinopathy, nephropathy, neurosis, ischemic cardiopathy, arteriosclerosis, and further a treatment and/or a preventive for obesity are provided.The invention relates to a compound of a formula (I): [wherein R1 and R2 represent a hydrogen, etc.; R3 represents a hydrogen atom, a halogen atom, etc.; R4 each independently represents a hydrogen atom, a lower alkyl group, etc.; Q represents a carbon atom, a nitrogen atom or a sulfur atom (the sulfur atom may be mono- or di-substituted with an oxo group); R5 and R6 each represent a hydrogen atom, a lower alkyl group, etc.; X1, X2, X3 and X4 each independently represent a carbon atom or a nitrogen atom; Z represents an oxygen atom, a sulfur atom or a nitrogen atom; Ar represents an aryl or heteroaryl group optionally mono to tri-substituted with a group selected from the substituent group β; ring A represents a 5- or 6-membered nitrogen-containing heteroaromatic group; m indicates an integer of from 1 to 6; n indicates an integer of from 0 to 3; p indicates an integer of from 0 to 2 (provided that at least two of X1 to X4 are carbon atoms); q indicates 0 or 1] or its pharmaceutically-acceptable salt, which has an effect of glucokinase activation and is useful as a treatment for diabetes.
摘要翻译：提供葡糖激酶活化剂; 提供糖尿病的治疗和/或预防，或治疗和/或预防糖尿病如视网膜病，肾病，神经症，缺血性心脏病，动脉硬化，以及进一步的治疗和/或预防肥胖症。本发明涉及式（I）的化合物：其中R 1和R 2代表氢等; R 3表示氢原子，卤素原子等; R 4各自独立地表示氢原子，低级烷基等; Q表示碳原子，氮原子或硫原子（硫原子可以被氧代基单取代或二取代）。 R 5和R 6各自表示氢原子，低级烷基等; X 1，X 2，X 3和X 4各自独立地表示碳原子或氮原子; Z表示氧原子，硫原子或氮原子; Ar表示任选被选自取代基组β的基团单取代至三取代的芳基或杂芳基; 环A表示5-或6-元含氮杂芳基; m表示1〜6的整数， n表示0〜3的整数， p表示0〜2的整数（条件是X 1〜X 4中的至少2个为碳原子）; q表示0或1]或其药学上可接受的盐，其具有葡糖激酶活化的作用，并且可用作糖尿病的治疗。

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